120891-11-4Relevant academic research and scientific papers
4-Bromo-2-(piperidin-1-yl)thiazol-5-yl-phenyl methanone (12b) inhibits Na+/K+-ATPase and Ras oncogene activity in cancer cells
Lefranc, Florence,Xu, Zhanjie,Burth, Patricia,Mathieu, Véronique,Revelant, Germain,Velho De Castro Faria, Mauro,Noyon, Caroline,Garcia, Diogo Gomes,Dufour, Damien,Bruyère, Céline,Gon?alves-De-Albuquerque, Cassiano Felippe,Van Antwerpen, Pierre,Rogister, Bernard,Hesse, Stéphanie,Kirsch, Gilbert,Kiss, Robert
, p. 213 - 223 (2013/07/25)
The in vitro growth inhibitory activity of 26 thiazoles (including 4-halogeno-2,5-disubtituted-1,3-thiazoles) and 5 thienothiazoles was assessed on a panel of 6 human cancer cell lines, including glioma cell lines. (4-Chloro-2-(piperidin-1-yl)thiazol-5-yl)(phenyl)methanone (12a) and (4-bromo-2-(piperidin-1-yl)thiazol-5-yl)(phenyl)methanone (12b) displayed ~10 times greater in vitro growth inhibitory activity than perillyl alcohol (POH), which therapeutically benefits glioma patients through the inhibition of both alpha-1 Na+/K+-ATPase (NAK) and Ras oncogene activity. The in vitro cytostatic activities (as revealed by quantitative videomicroscopy) displayed by 12a and 12b were independent of the intrinsic resistance to pro-apoptotic stimuli associated with cancer cells. Compounds 12a and 12b displayed relatively similar inhibitory activities on purified guinea pig brain preparations that mainly express NAK alpha-2 and alpha-3 subunits, whereas only compound 12b was efficacious against purified guinea pig kidney preparations that mainly express the NAK alpha-1 subunit, which is also expressed in gliomas, melanomas and non-small-cell lung cancers NSCLCs.
Azoles. Part 10. Thiazolothienopyrimidine, a New Heterocyclic Ring System
Athmani, Salah,Iddon, Brian
, p. 7689 - 7702 (2007/10/02)
Thienothiazoles were prepared by reaction of 4-chlorothiazole-5-carbaldehydes or 4-chlorothiazole-5-carbonitriles with either ethyl 2-mercaptoacetate or 2-mercaptoacetamide.The 6-aminothienothiazole-5-carboxamides obtained were converted int
New thiazole compounds having fungicidal activity
-
, (2008/06/13)
The invention relates to new thiazole compounds of the general formula STR1 wherein R is an C1 -C12 alkyl group or a phenyl group, which groups are unsubstituted or substituted with halogen, nitro or cyano; R1 is a cyano group; a formyl group; an alkylcarbonyl or alkoxycarbonyl group having 2-5 carbon atoms; or a substituted or non-substituted benzoyl group; R2 is a hydrogen atom; a halogen atom; an amino group; an amino group substituted with 1 or 2 substituents selected from the group consisting of C1 -C4 alkyl, C2 -C5 alkynyl, C2 -C5 alkylcarbonyl and C2 -C5 alkoxycarbonyl; an alkyl, alkoxy, alkylthio, alkylsulphinyl or alkyl-sulphonyl group having 1-4 carbon atoms; or a substituted or non-substituted aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl group; and n is 1 or 2. The new compounds show a fungicidal activity and may be used in particular against plant pathogenic seed fungi and soil fungi.
